Technical Field
The present invention relates to an aqueous composition and the like.
Related Art
Halo-isoquinoline derivatives such as ripasudil (chemical name:
4-fluoro-5-{[(2S)-2-methyl-1,4-diazepan-1-yl]sulfonyl}isoquinoline) of the following formula:
and4-bromo-5-{[(2S)-2-methyl-1,4-diazepan-1-yl]sulfonyl}isoquinoline of the following formula:
are known to have pharmacological activity such as Rho kinase-inhibitory activity (e.g., JP 4212149 B1 and WO 2006/115244 A) and to be useful for preventing or treating eye diseases. Specifically, for example, they are reported to be useful for preventing or treating ocular hypertension and glaucoma (e.g., WO 2006/068208 A) or for preventing or treating ocular fundus diseases such as age-related macular degeneration (e.g., JP 5557408 B1).
It is therefore very useful to establish a technology for stably formulating these halo-isoquinoline derivatives into, for example, preparations for ophthalmic application.
JP 4972552 B1 discloses that ripasudil ((S)-(−)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine) or a salt thereof is administered in combination with brinzolamide, which is a carbonic anhydrase inhibitor. However, JP 4972552 B1 simply discloses that a solution containing 0.5% of ripasudil and an ophthalmic solution containing 1% of brinzolamide are sequentially dropped into the same eye of a rabbit. JP 4972552 B1 does not disclose at all an aqueous composition containing both of these compounds, storage of such an aqueous composition in a container, or storage stability of such an aqueous composition in a container over time.